Discovery of METTL3 small molecule inhibitors by virtual screening of natural products

Y Du, Y Yuan, L Xu, F Zhao, W Wang, Y Xu… - Frontiers in …, 2022 - frontiersin.org
N6-Methyladenosine (m6A) is the most prevalent mRNA modification in mammalian cells
that is mainly catalyzed by the methyltransferase complex of methyltransferase-like 3 and …

METTL3 from target validation to the first small-molecule inhibitors: a medicinal chemistry journey

F Fiorentino, M Menna, D Rotili… - Journal of Medicinal …, 2023 - ACS Publications
RNA methylation is a critical mechanism for regulating the transcription and translation of
specific sequences or for eliminating unnecessary sequences during RNA maturation …

Roles and drug development of METTL3 (methyltransferase-like 3) in anti-tumor therapy

P Xu, R Ge - European journal of medicinal chemistry, 2022 - Elsevier
Methyltransferase complex, such as METTL3/METTL14/WTP, catalyze N 6-methyladenosine
(m 6 A), which is the most abundant mRNA modification in mammals. Besides acting as am …

[HTML][HTML] METTL3 plays multiple functions in biological processes

S Liu, L Zhuo, J Wang, Q Zhang, Q Li, G Li… - American journal of …, 2020 - ncbi.nlm.nih.gov
Abstract N 6-methyladenosine (m 6 A) is the most common internal modification of mRNAs
in higher eukaryotic. This process is performed by methyltransferase. Methyltransferase-like …

Novel insights into the m6A-RNA methyltransferase METTL3 in cancer

Y Cai, R Feng, T Lu, X Chen, X Zhou, X Wang - Biomarker Research, 2021 - Springer
Abstract N6-methyladenosine (m 6 A) is a prevalent internal RNA modification in higher
eukaryotic cells. As the pivotal m 6 A regulator, RNA methyltransferase-like 3 (METTL3) is …

METTL3 inhibitors for epitranscriptomic modulation of cellular processes

EV Moroz‐Omori, D Huang, R Kumar Bedi… - …, 2021 - Wiley Online Library
The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification
of RNA. Using a structure‐based drug discovery approach, we identified a METTL3 inhibitor …

Mining for METTL3 inhibitors to suppress cancer

J Li, RI Gregory - Nature structural & molecular biology, 2021 - nature.com
The RNA methyltransferase METTL3 catalyzes N 6-methyladenosine (m6A) modification of
messenger RNAs (mRNAs). It is overexpressed in many types of cancer, including acute …

METTL3 promotes the proliferation and mobility of gastric cancer cells

S Lin, J Liu, W Jiang, P Wang, C Sun, X Wang… - Open …, 2019 - degruyter.com
Abstract Methyltransferase-like 3 (METTL3) was originally known to be responsible for N6-
methyladenosine (m6A) modification of mRNA. Recent studies have found that METTL3 …

Discovery of substituted indole derivatives as allosteric inhibitors of m6A‐RNA methyltransferase, METTL3‐14 complex

JH Lee, S Kim, MS Jin, YC Kim - Drug Development Research, 2022 - Wiley Online Library
Abstract m6A RNA methyltransferase (METTL3‐14) catalyzes the methylation of adenosine
in mRNA and plays important roles in mRNA functions, and it has been implicated in the …

Functions, mechanisms, and therapeutic implications of METTL14 in human cancer

Q Guan, H Lin, L Miao, H Guo, Y Chen, Z Zhuo… - Journal of hematology & …, 2022 - Springer
RNA modification plays a crucial role in many biological functions, and its abnormal
regulation is associated with the progression of cancer. Among them, N6-methyladenine …